Abstract

The active compounds, cis-3-(2',4',5'-trimethoxyphenyl)-4-{(E)-2''',4''',5'''-trimethoxystyryl}cyclohex-1-ene (Compound C) and (E)-4-(3',4'-dimethoxyphenyl)but-3-en-1-ol (Compound D), have been identified in hexane fraction of Zingiber cassumunar Roxb., the medicinal plant which has been used for pain relief in arthritis including osteoarthritis (OA) and rheumatoid arthritis (RA). It was therefore interesting to investigate the chondroprotective activity of these compounds in vitro. Articular cartilage explants were cultured in the culture media containing 7 ng/ml of interleukin-1β (IL-1β), in the presence or absence of Compound C or Compound D at the concentration range of 1 to 100 μM. It was found that these compounds at concentrations of 10 and 100 μM significantly inhibited the IL-1β-induced cartilage degeneration by conserving the content of the cartilage matrix biomolecules such as collagen and uronic acid (UA) within the cartilage explants; and also resulted in the decline of releasing sulfated glycosaminoglycans and hyaluronic acid (HA) into the culture media. The increase in activities of matrix metalloproteinase-2 (MMP-2) and MMP-13 caused by IL-1β was significantly diminished by Compound C and Compound D. Additionally, the results showed no significant difference between the two active constituents and diacerein, an anti-arthritic agent used in OA, in those activities at a concentration of 100 μM. This is a pioneering evidence that indicate the potential chondroprotective property of the Z. cassumunar active compounds.

Key words: Zingiber cassumunar, chondroprotective activity, cartilage explant, rheumatoid arthritis, osteoarthritis, cis-3-(2',4',5'-trimethoxyphenyl)-4-{(E)-2''',4''',5'''-trimethoxystyryl}cyclohex-1-ene, (E)-4-(3',4'-dimethoxyphenyl)but-3-en-1-ol.